Shi Xiang, Guan Ruowei, Zhou Lutan, Zuo Zhichuang, Tao Xuelin, Wang Pin, Zhou Yanrong, Yin Ronghua, Zhao Longyan, Gao Na, Zhao Jinhua
School of Pharmaceutical Sciences, South-Central University for Nationalities, Wuhan 430074, China.
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China.
Mar Drugs. 2021 Mar 18;19(3):162. doi: 10.3390/md19030162.
Unique fucosylated glycosaminoglycans (FG) have attracted increasing attention for various bioactivities. However, the precise structures of FGs usually vary in a species-specific manner. In this study, HfFG was isolated from and purified by anion exchange chromatography with the yield of ~0.9%. HfFG was composed of GlcA, GalNAc and Fuc, its molecular weight was 47.3 kDa, and the -OSO/-COO molar ratio was 3.756. HfFG was depolymerized by a partial deacetylation-deaminative cleavage method to obtain the low-molecular-weight HfFG (dHfFG). Three oligosaccharide fragments (Fr-1, Fr-2, Fr-3) with different molecular weights were isolated from the dHfFG, and their structures were revealed by 1D and 2D NMR spectroscopy. HfFG should be composed of repeating trisaccharide units -{(L-FucS-α1,3-)d-GlcA-β1,3-d-GalNAc-β1,4-}-, in which sulfated fucose (FucS) includes Fuc, Fuc and Fuc residues linked to O-3 of GlcA in a ratio of 45:35:20. Furthermore, the heparanase inhibitory activities of native HfFG and oligosaccharide fragments (Fr-1, Fr-2, Fr-3) were evaluated. The native HfFG and its oligosaccharides exhibited heparanase inhibitory activities, and the activities increased with the increase of molecular weight. Additionally, structural characteristics such as sulfation patterns, the terminal structure of oligosaccharides and the presence of fucosyl branches may be important factors affecting heparanase inhibiting activity.
独特的岩藻糖基化糖胺聚糖（FG）因其多种生物活性而受到越来越多的关注。然而，FG的精确结构通常因物种而异。在本研究中，通过阴离子交换色谱从[具体来源未给出]中分离并纯化出HfFG，产率约为0.9%。HfFG由GlcA、GalNAc和Fuc组成，其分子量为47.3 kDa，-OSO/-COO摩尔比为3.756。通过部分脱乙酰化-脱氨基裂解方法对HfFG进行解聚，以获得低分子量的HfFG（dHfFG）。从dHfFG中分离出三个不同分子量的寡糖片段（Fr-1、Fr-2、Fr-3），并通过一维和二维核磁共振光谱揭示了它们的结构。HfFG应由重复的三糖单元-{(L-FucS-α1,3-)d-GlcA-β1,3-d-GalNAc-β1,4-}-组成，其中硫酸化岩藻糖（FucS）包括以45:35:20的比例与GlcA的O-3相连的Fuc、Fuc和Fuc残基。此外，还评估了天然HfFG和寡糖片段（Fr-1、Fr-2、Fr-3）的乙酰肝素酶抑制活性。天然HfFG及其寡糖表现出乙酰肝素酶抑制活性，且活性随分子量的增加而增加。此外，硫酸化模式、寡糖的末端结构和岩藻糖基分支的存在等结构特征可能是影响乙酰肝素酶抑制活性的重要因素。
